Dual receptor blockade by bosentan: clinical experience in treatment of pulmonary hypertension

Susana Hoette^1,2, Dermot S O’Callaghan², Carlos Jardim¹, Rogerio Souza^1
1Pulmonary Circulation Unit, Pulmonary Department, Heart Institute, University of São Paulo Medical School, Sao Paulo, Brazil; ²Hôpital Antoine Béclère, Université Paris Sud, Orsay, France

Abstract: Pulmonary hypertension is characterized by an increase in mean pulmonary arterial pressure and right ventricular overload. Endothelin-1 (ET-1) is a potent vasoconstrictor with an important role in the pathogenesis of pulmonary hypertension. In addition to its vasoconstrictive action, ET-1 also stimulates cell proliferation, fibrosis, and inflammation. The blockade of both receptors involved in the action of ET-1 is beneficial in the treatment of pulmonary hypertension. The use of endothelin dual receptor blockade leads to improvements in quality of life, functional capacity, and pulmonary hemodynamics in affected patients. This article reviews the importance of ET-1 in the pathogenesis of pulmonary hypertension and demonstrates the benefits of blockage of the action of ET-1 in this disease.

Keywords: pulmonary hypertension treatment, endothelin-1, endothelin receptor blockage, bosentan